化合物BMS-986278 T39647

Product Introduction
Bioactivity


英文名: BMS-986278

描述: BMS-986278 是一种具有口服活性和高效性的血磷脂酸受体 1 (LPA1) 拮抗剂，对人和小鼠 LPA1 的 Kb 值分别为 6.9 nM 和 4.0 nM。BMS-986278 可用于研究用于特发性肺纤维化。

体外活性: With Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively, BMS-986278 is a high-affinity LPA1 antagonist. These values were determined in CHO cells overexpressing LPA1[1]. BMS-986278 also antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, exhibiting a Kb of 5.8 nM[1].

体内活性: In CD1 mice, a single oral administration of BMS-986278 (0.1-10 mg/kg) completely inhibits LPA-stimulated systemic histamine release in a concentration-dependent manner[1]. Furthermore, when administered orally twice daily for 14 days at doses ranging from 3 to 30 mg/kg, BMS-986278 reduces Bleomycin-induced collagen deposition and lung fibrosis in rats[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 90 mg/mL (202.02 mM)


关键字: BMS-986278 | BMS986278 | BMS 986278

相关产品: ASP6432 | ONO-7300243 | TAK-615 | LPA2 antagonist 2 | TC LPA5 4 | DBIBB | LPA1 receptor antagonist 1 | GRI977143 | Edg-2 receptor inhibitor 1 | BMS-986020

相关库: Drug Repurposing Compound Library | Membrane Protein-targeted Compound Library | GPCR Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途